Table 9SAR Analysis on the Eastern Ring: Influence of Other Substituents

Entry No.CID
SID
Broad ID
*
Image ml281fu8.jpg
Potency (μM)
Mean ± S.E.M.
(n=replicates)
Fold Selectivity
STK33PKA
R1nIC50nIC50
16205077
125081938
BRD-K21654006
S
Image ml281fu58.jpg
4> 102> 10NA
Solubility (PBS): <0.5 μM, Purity: 100%
253347980
125081963
BRD-K13799318
S
Image ml281fu59.jpg
4> 102> 10NA
Solubility (PBS): 4.0 μM, Purity: 78%
353347973
125081940
BRD-K53926138
S
Image ml281fu60.jpg
4> 102> 10NA
Solubility (PBS): <0.5 μM, Purity: 100%
453347983
125081965
BRD-K31872678
S
Image ml281fu61.jpg
4> 102> 10NA
Solubility (PBS): <0.5 μM, Purity: 100%
553347985
125081968
BRD-K62009824
S
Image ml281fu62.jpg
4> 102> 10NA
Solubility (PBS): 56.6 μM, Purity: 83%
653348002
125081975
BRD-K29894029
S
Image ml281fu63.jpg
4> 102> 10NA
Solubility (PBS): <0.5 μM, Purity: 100%

NA=Not applicable;

*

P=purchased; S=synthesized

From: Screen for Inhibitors of STK33 Kinase Activity

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Probe Reports from the NIH Molecular Libraries Program [Internet].

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